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Assay Detail

CHEMBL3390676

Review assay metadata, readout intent, target linkage, and publication context from the same page.

ADMET
Inhibition of CYP2D6 (unknown origin) using bufuralol substrate
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Na(v)1.7.
Sun S, Jia Q, Zenova AY, Chafeev M, Zhang Z, Lin S, Kwan R, Grimwood ME, Chowdhury S, Young C, Cohen CJ, Oballa RM.
Bioorg Med Chem Lett (2014) 24 : 4397 -4401
PubMed 25176194 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.58 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3325526 1 6.58
CHEMBL3325537 1 6.57
CHEMBL3325551 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3325526 IC50 = 260.0 nM 6.58
CHEMBL3325537 IC50 = 270.0 nM 6.57
CHEMBL3325551 IC50 > 10000.0 nM -